The discovery and application of antibiotics was one of the greatest achievements in the field of medicaments in the 20th century, which can be regarded as a revolutionary discovery in the process of fighting against diseases. From then on, medical field entered a golden age for significant reduction in the incidence rate of bacterial diseases. However, due to the extensive use and even abuse of antibiotics, the efficacy thereof is weakening as the drug resistance of bacteria is becoming increasingly serious, and thus the “Age of Post-Antibiotics” is coming closer. A number of new drug-resistant strains have been found clinically, among which MRSA (methicillin-resistant staphylococcus aureus), VRE (vancomycin-resistant enterococci), PRSP (penicillin-resistant streptococcus pneumoniae), and the like have made the clinical treatment rather difficult, because there are only a few kinds of therapeutic medicines against them.
Linezolid is an oxazolidinone compound that was put into the market in the United States in 2000. In clinic, Linezolid is mainly utilized to treat nosocomial pneumonia, soft tissue infections, etc., and is also useful in cure of surgical infectious diseases. In addition, Linezolid displays excellent pharmacokinetic characteristics such as high tissue drug concentration in skeleton, lung, cerebrospinal fluid, etc., and exhibits excellent permeability into infectious bacteria cells. There continues to be interest in discovering and developing novel oxazolidinone medicine candidates.